Determination of Aloesin in Rat Plasma by LC-MS/MS and Its Pharmacokinetic Study
- VernacularTitle:LC-MS/MS法测定大鼠血浆中芦荟苦素浓度及其药动学研究
- Author:
Yinfeng TAN
1
;
Moxiao SUN
1
;
Lei ZHANG
1
;
Wenyue YANG
1
;
Hailong LI
1
;
Youbin LI
1
Author Information
1. School of Pharmacy,Hainan Medical University/Hainan Provincial Key Laboratory for Research and Development of Tropical Herbs/Haikou Key Labora tory of Li Nati onality Medicine,Haikou 571159,China
- Publication Type:Journal Article
- Keywords:
Aloesin;
Aloeresin D;
Plasma concentration
- From:
China Pharmacy
2021;32(22):2701-2705
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE:To establish a method for the determination of aloesin in plasma of rats ,and to investigate pharmacokinetic characteristics of aloesin. METHODS :The plasma samples were precipitated with methanol. Using aloeresin D as internal standard ,the plasma concentration of aloesin was determined by LC-MS/MS. The determination was performed on Synergi Hydro-RP column with mobile phase consisted of 0.1‰ formic acid-methanol (gradient elution )at the flow rate of 0.50 mL/min. The column temperature was 30 ℃,and sample size was 5 µL. The electrospray ionization source was applied to carry out negative ion detection with multiple reaction monitoring mode . The ion transitions for quantitative analysis were m/z 393.1→272.9(aloesin) and m/z 555.3→144.9(internal standard ),respectively. The concentration of aloesin in venous blood was determined by above method at 0.083,0.167,0.333,0.667,1,1.5,2.5,4,6,8,10 h after intravenous injection (3.35 mg/kg)and intragastric administration(16.75 mg/kg)of aloesin. DAS 3.0 software was used to calculate pharmacokinetic parameters. RESULTS :The linear range of aloesin were 1-600 ng/mL(r=0.994 5). The lower limit of quantification was 1 ng/mL,and RSDs of within and between batches were less than 15%;accuracies within and between batches were within ±15%. The matrix factors were (92.74± 4.33)%-(94.84±2.57)%,and extraction recoveries were (69.04±2.13)%-(75.03±2.84)%;the deviation between the measured results of the stability test and the theoretical values were within ±15%. After intravenous injection and intragastric administration of aloesin ,main pharmacokinetic parameters were as follows :cmax were(10 693.3±2 745.3)and(223.3±36.2)ng/mL;t1/2 were (2.45±1.45)and(3.33±1.91)h;AUC0-24h were(4 190.6±883.6)and(1 210.1±93.9)ng·h/mL(n=3). Absolute bioavailabi- lity was 11.13%. CONCLUSIONS :The established method is rapid and sensitive for plasma determination of aloesin ,and suitable for its pharmacokinetic study.